title: Activation and inhibition of leukotriene A4 hydrolase aminopeptidase activity by diphenyl ether and derivatives.
abstract: The synthesis and biological evaluation of a series of diphenyl ether derivatives were described. The compounds can either activate or inhibit the aminopeptidase activity of leukotriene A(4) hydrolase, while at the same time do not influence the hydrolase activity. Further enzyme kinetics and molecular modeling investigation on these novel chemical activators revealed their possible activation mechanism. These compounds can be used as probes to regulate the aminopeptidase activity of leukotriene A(4) hydrolase.
authors.affiliation: Beijing National Laboratory for Molecular Sciences, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
authors.forename: Xiaolu
authors.initials: X
authors.lastname: Jiang
authors.forename: Lu
authors.initials: L
authors.lastname: Zhou
authors.forename: Dengguo
authors.initials: D
authors.lastname: Wei
authors.forename: Hu
authors.initials: H
authors.lastname: Meng
authors.forename: Ying
authors.initials: Y
authors.lastname: Liu
authors.forename: Luhua
authors.initials: L
authors.lastname: Lai
mesh_terms: D002626:Chemistry, Pharmaceutical; D015195:Drug Design; D004789:Enzyme Activation; D004851:Epoxide Hydrolases / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D006801:Humans; D006868:Hydrolysis; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008956:Models, Chemical; D008958:Models, Molecular; D008968:Molecular Conformation; D010647:Phenyl Ethers / Q000737:chemistry*; D011485:Protein Binding; D013379:Substrate Specificity
chemical_list: D010647:Phenyl Ethers; C031538:phenyl ether; D004851:Epoxide Hydrolases; C043134:leukotriene A4 hydrolase